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AS2521780

Chemical Structure : AS2521780

CAS No.: 1214726-89-2

AS2521780 (AS 2521780;AS-2521780)

Catalog No.: PC-60994Not For Human Use, Lab Use Only.

AS2521780 is a potent, selective, orally bioavailable PKCθ inhibitor that inhibits combinant human PKCθ enzyme with IC50 of 0.48 nM, >30-fold higher than other PKC isoforms.

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Biological Activity

AS2521780 is a potent, selective, orally bioavailable PKCθ inhibitor that inhibits combinant human PKCθ enzyme with IC50 of 0.48 nM, >30-fold higher than other PKC isoforms; also displays >100-fold selectivity over a panel of 27 protein kinases (100-fold over CDK2, IC50=84 nM); suppresses CD3/CD28-induced IL-2 gene transcription (IC50=14 nM) in Jurkat T cells and proliferation of human primary T cells (IC50=17 nM), also suppresses concanavalin A-induced cytokine production by rat splenocytes and monkey PBMCs with similar potency; potentially ameliorate T cell-mediated autoimmune diseases in vivo models.

Physicochemical Properties

M.Wt 547.766
Formula C30H41N7OS
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-({[(1R,3R,4s,5S)-4-{[(trans-4-hydroxycyclohexyl) methyl]amino}adamantan-1-yl]methyl}amino)-2-({[2-(methylsulfanyl)pyridin-3-yl]methyl}amino)pyrimidine-5-carbonitrile

References

1. Fukahori H, et al. Eur J Pharmacol. 2014 Dec 15;745:217-22.

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